Preferred Label : NEDD8 Activating Enzyme E1 Inhibitor TAS4464;
NCIt synonyms : NAE Inhibitor TAS4464;
NCIt definition : An inhibitor of NEDD8 (neural precursor cell expressed, developmentally down-regulated
8) activating enzyme E1 (NAE), with potential antineoplastic activity. Upon administration,
TAS4464 selectively binds to and inhibits NAE, which prevents NAE/NEDD8-mediated signaling
and prevents the NEDD8 conjugation of cullin-RING ligase complexes (CRLs). This inactivates
the CRLs leading to an accumulation of CRL substrate proteins, such as CDT1, p27,
p21 and phosphorylated IkappaB, and inactivates nuclear factor-kappaB (NF-kB) as well
as downregulates anti-apoptotic proteins. This causes cell cycle dysregulation, induces
apoptosis, and inhibits tumor cell proliferation and survival. NAE catalyzes the first
step in the NEDD8 conjugation (neddylation) pathway which controls cancer cell growth
and survival through activation of CRLs.;
Molecule name : TAS4464;
NCI Metathesaurus CUI : CL523721;
Origin ID : C136418;
UMLS CUI : C4526664;
Semantic type(s)
- UMLS correspondences (same concept)
- TAS4464 [MeSH Supplementary Concept]
- concept_is_in_subset
- has_target
